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首页> 外文期刊>Pharmaceutical research >Monitoring microviscosity and microacidity of the albumin microenvironment inside degrading microparticles from poly(lactide-co-glycolide) (PLG) or ABA-triblock polymers containing hydrophobic poly(lactide-co-glycolide) A blocks and hydrophilic poly(
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Monitoring microviscosity and microacidity of the albumin microenvironment inside degrading microparticles from poly(lactide-co-glycolide) (PLG) or ABA-triblock polymers containing hydrophobic poly(lactide-co-glycolide) A blocks and hydrophilic poly(

机译：监测降解包含疏水聚（丙交酯-乙交酯）A嵌段和亲水性聚（丙交酯-乙交酯）的聚（丙交酯-共-乙交酯）（PLG）或ABA-三嵌段聚合物微粒的白蛋白微环境内部的微粘度和微酸度

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PURPOSE: The purpose of this study was to monitor the microenvironment of an encapsulated model protein during the release from biodegradable microparticles (MP) made from three different polymers, namely poly(lactide-co-glycolide) (PLG) and ABA-triblock polymers containing hydrophobic poly(lactide-co-glycolide) A blocks and hydrophilic poly(ethyleneoxide) B blocks with an A:B ratio of 90:10 (ABA1O) and 70:30 (ABA30). METHODS: MP loaded with spin labeled albumin were prepared by a w/o/w technique. The particles were characterized by light scattering and electron microscopy. In vitro release of albumin was determined by size exclusion chromatography. Light microscopic experiments were conducted to visualize water penetration in the matrix. The protein microenvironment inside the degrading microparticles was characterized noninvasively by 2 GHz EPR spectroscopy. RESULTS: Water penetrated rapidly into all MP in the range of few minutes. A burst release was observed for PLG. The release from ABA block-polymers continued for over 14 days despite the rapid solubilization of the protein inside the microparticles. The initial microviscosity of the protein environment inside the ABA particles after exposure to buffer was 2 mm2/s and increased with time. A gradual decrease of the pH to a value of 3.5 was observed within the MP. CONCLUSIONS: The data indicate that the microviscosity and microacidity inside protein loaded microparticles can be studied nondestructively by EPR spectroscopy. Our results clearly demonstrate that ABA-block polymers are superior to PLG allowing a controlled release of proteins from swollen microspheres.
机译：目的：本研究的目的是监测由三种不同聚合物制成的可生物降解微粒（MP）释放过程中包封的模型蛋白的微环境，这三种聚合物分别是聚丙交酯-共-乙交酯（PLG）和ABA-三嵌段聚合物疏水聚（丙交酯-乙交酯）A嵌段和亲水性聚（环氧乙烷）B嵌段，其A：B比为90:10（ABA10）和70:30（ABA30）。方法：采用w / o / w技术制备载有自旋标记白蛋白的MP。通过光散射和电子显微镜对颗粒进行表征。通过尺寸排阻色谱法测定白蛋白的体外释放。进行光学显微镜实验以可视化水在基质中的渗透。降解微粒内部的蛋白质微环境通过2 GHz EPR光谱进行了非侵入式表征。结果：水在几分钟内迅速渗透到所有MP中。观察到PLG突然释放。尽管微粒内部蛋白质迅速溶解，但从ABA嵌段聚合物中释放仍持续1​​4天以上。暴露于缓冲液后，ABA颗粒内部蛋白质环境的初始微粘度为2 mm2 / s，并随时间增加。在MP内观察到pH值逐渐降低至3.5。结论：数据表明，可通过EPR光谱无损研究蛋白质负载微粒内部的微粘度和微酸度。我们的结果清楚地表明，ABA嵌段聚合物优于PLG，可以从溶胀的微球中控制释放蛋白质。

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